Issue 4, 2021

Chemical modulation of Kv7 potassium channels

Abstract

The rising interest in Kv7 modulators originates from their ability to evoke fundamental electrophysiological perturbations in a tissue-specific manner. A large number of therapeutic applications are, in part, based on the clinical experience with two broad-spectrum Kv7 agonists, flupirtine and retigabine. Since precise molecular structures of human Kv7 channel subtypes in closed and open states have only very recently started to emerge, computational studies have traditionally been used to analyze binding modes and direct the development of more potent and selective Kv7 modulators with improved safety profiles. Herein, the synthetic and medicinal chemistry of small molecule modulators and the representative biological properties are summarized. Furthermore, new therapeutic applications supported by in vitro and in vivo assay data are suggested.

Graphical abstract: Chemical modulation of Kv7 potassium channels

Article information

Article type
Review Article
Submitted
23 Sep 2020
Accepted
01 Dec 2020
First published
14 Jan 2021

RSC Med. Chem., 2021,12, 483-537

Author version available

Chemical modulation of Kv7 potassium channels

M. Borgini, P. Mondal, R. Liu and P. Wipf, RSC Med. Chem., 2021, 12, 483 DOI: 10.1039/D0MD00328J

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